General Information of DTT (ID: TTLA931)

DTT Name Neuronal acetylcholine receptor alpha-7 (CHRNA7) DTT Info
Gene Name CHRNA7

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Approved Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Investigative Drug(s)
2 Approved Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
ALCURONIUM DM2U4XQ Anaesthesia 9A78.6 Approved [1]
Ziprasidone DMM58JY Bipolar disorder 6A60 Approved [2]
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14 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
AMG 386 DMQJXL4 Breast cancer 2C60-2C65 Phase 3 [3]
CYTISINE DMUF0BJ Tobacco dependence 6C4A.2 Phase 3 [4]
EVP-6124 DMLQO7F Alzheimer disease 8A20 Phase 3 [5]
ABT-126 DM2OS51 Alzheimer disease 8A20 Phase 2 [6]
AQW-051 DMD2RFO Alzheimer disease 8A20 Phase 2 [7]
Bradanicline DMZEECF Chronic cough MD12 Phase 2 [8]
GTS-21 DMEN5KA Parkinson disease 8A00.0 Phase 2 [9]
JNJ-39393406 DMUOEKM Depression 6A70-6A7Z Phase 2 [10]
MEM-3454 DMPNDYU Schizophrenia 6A20 Phase 2 [2]
TC-6987 DMNFP21 Asthma CA23 Phase 2 [11]
AVL-3288 DMGAKR9 Cognitive impairment 6D71 Phase 1 [12]
BMS-933043 DMG3J6C Psychiatric disorder 6E8Z Phase 1 [13]
BNC375 DMI4UY3 Cognitive impairment 6D71 Phase 1 [14]
R4996 DMSKHIC Neurological disorder 6B60 Phase 1 [3]
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⏷ Show the Full List of 14 Clinical Trial Drug(s)
4 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
AZD-9684 DMHA5ME Thrombosis DB61-GB90 Discontinued in Phase 2 [15]
AZD0328 DM4B7CM Alzheimer disease 8A20 Discontinued in Phase 2 [16]
ABT-107 DMPCYV6 Attention deficit hyperactivity disorder 6A05.Z Discontinued in Phase 1 [17]
PNU-282987 DMGDC36 Schizophrenia 6A20 Terminated [2]
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2 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
PHA-568487 DMM149N Cognitive impairment 6D71 Preclinical [18]
RMG-40083 DMJGQD2 Schizophrenia 6A20 Preclinical [2]
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24 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
3,8-dibromoboldine DM23CEI Discovery agent N.A. Investigative [19]
3-bromoboldine DMPF7O2 Discovery agent N.A. Investigative [19]
4BP-TQS DMS0JVE Discovery agent N.A. Investigative [20]
A-582941 DM7R8DJ Discovery agent N.A. Investigative [21]
A-867744 DM96F8U Discovery agent N.A. Investigative [22]
AZD-6319 DMD4YO9 Alzheimer disease 8A20 Investigative [23]
Barbituric acid derivative DM2I19P Discovery agent N.A. Investigative [24]
CP-810123 DMXDG13 Discovery agent N.A. Investigative [25]
EVP-4473 DMHMFKE Alzheimer disease 8A20 Investigative [23]
GCCSHPACAGNNQHIC* DM4BZEC Discovery agent N.A. Investigative [26]
GCCSNPVCHLEHSNLC* DMJ0ICN Discovery agent N.A. Investigative [26]
JN-711 DMFU76I Central nervous system disease 8A04-8D87 Investigative [23]
JNJ-1930942 DMKH9O7 Cognitive impairment 6D71 Investigative [23]
LY2087101 DMIS82X Discovery agent N.A. Investigative [27]
NS1738 DM2S5ZF Discovery agent N.A. Investigative [28]
PH-709829 DM5GY6Z Discovery agent N.A. Investigative [29]
PheTQS DMWMBP3 Central nervous system disease 8A04-8D87 Investigative [23]
PNU-120596 DMYBQM7 Discovery agent N.A. Investigative [30]
PSAB-OFP DM38JMK Discovery agent N.A. Investigative [31]
TOXIFERINE DMJHTQK Discovery agent N.A. Investigative [1]
[125I]epibatidine DMZWQH3 Discovery agent N.A. Investigative [23]
[3H]A-585539 DMSDY2Z Discovery agent N.A. Investigative [32]
[3H]AZ11637326 DMPVG5Y Discovery agent N.A. Investigative [33]
[3H]methyllycaconitine DMYWGCS Discovery agent N.A. Investigative [23]
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⏷ Show the Full List of 24 Investigative Drug(s)
Molecule Interaction Atlas

References

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2 The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
3 Clinical pipeline report, company report or official report of Roche (2009).
4 3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4889-97.
5 Normalizing effects of EVP-6124, an alpha-7 nicotinic partial agonist, on event-related potentials and cognition: a proof of concept, randomized trial in patients with schizophrenia. J Psychiatr Pract. 2014 Jan;20(1):12-24.
6 A phase 2 randomized, controlled trial of the alpha7 agonist ABT-126 in mild-to-moderate Alzheimer's dementia. Alzheimer's & Dementia: Translational Research & Clinical Interventions Volume 1, Issue 1, June 2015, Pages 81-90.
7 AQW051, a novel and selective nicotinic acetylcholine receptor alpha7 partial agonist, reduces l-Dopa-induced dyskinesias and extends the duration of l-Dopa effects in parkinsonian monkeys. Parkinsonism Relat Disord. 2014 Nov;20(11):1119-23.
8 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight
9 The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21). Behav Brain Res. 2000 Aug;113(1-2):169-81.
10 Allosteric alpha-7 nicotinic receptor modulation and P50 sensory gating in schizophrenia: a proof-of-mechanism study. Neuropharmacology. 2013 Jan;64:197-204.
11 ClinicalTrials.gov (NCT01293669) Glycemic Control, Safety and Tolerability of TC-6987 Monotherapy in Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
12 Differential immediate and sustained memory enhancing effects of alpha7 nicotinic receptor agonists and allosteric modulators in rats. PLoS One. 2011;6(11):e27014.
13 Clinical pipeline report, company report or official report of Phrma.org Alzheimers 2012.
14 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
15 Blockade and activation of the human neuronal nicotinic acetylcholine receptors by atracurium and laudanosine. Anesthesiology. 2001 Apr;94(4):643-51.
16 Ultra-low exposure to -7 nicotinic acetylcholine receptor partial agonists elicits an improvement in cognition that corresponds with an increase in -7 receptor expression in rodents: implications for low dose clinical efficacy.Neuroscience.2011 Jul 14;186:76-87.
17 In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107. J Pharmacol Exp Ther. 2010 Sep 1;334(3):863-74.
18 Multiple species metabolism of PHA-568487, a selective alpha 7 nicotinic acetylcholine receptor agonist. Drug Metab Lett. 2010 Aug;4(3):162-72.
19 Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers. Bioorg Med Chem. 2007 May 15;15(10):3368-72.
20 Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site. Proc Natl Acad Sci U S A. 2011 Apr 5;108(14):5867-72.
21 Broad-spectrum efficacy across cognitive domains by alpha7 nicotinic acetylcholine receptor agonism correlates with activation of ERK1/2 and CREB phosphorylation pathways. J Neurosci. 2007 Sep 26;27(39):10578-87.
22 In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methy... J Pharmacol Exp Ther. 2009 Jul;330(1):257-67.
23 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 468).
24 Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57.
25 Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor ag... J Med Chem. 2010 Feb 11;53(3):1222-37.
26 Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. J Med Chem. 2005 Jul 28;48(15):4705-45.
27 Identification and pharmacological profile of a new class of selective nicotinic acetylcholine receptor potentiators. J Pharmacol Exp Ther. 2006 Sep;318(3):1108-17.
28 An allosteric modulator of the alpha7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J Pharmacol Exp Ther. 2007 Oct;323(1):294-307.
29 Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor:... Bioorg Med Chem Lett. 2008 Jun 15;18(12):3611-5.
30 A novel positive allosteric modulator of the alpha7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J Neurosci. 2005 Apr 27;25(17):4396-405.
31 PSAB-OFP, a selective alpha 7 nicotinic receptor agonist, is also a potent agonist of the 5-HT3 receptor. Eur J Pharmacol. 2002 Oct 4;452(2):137-44.
32 [3H]A-585539 [(1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane], a novel high-affinity alpha7 neuronal nicotinic... J Pharmacol Exp Ther. 2008 Jan;324(1):179-87.
33 In vitro binding characteristics of [3H]AZ11637326, a novel alpha7-selective neuronal nicotinic receptor agonist radioligand. Eur J Pharmacol. 2010 Oct 25;645(1-3):63-9.